AUTHOR=Souza Julia M. , de Carvalho Érica A. A. , Candido Ana Carolina B. B. , de Mendonça Rafael P. , Fernanda da Silva Maria , Parreira Renato L. T. , Dias Fernanda G. G. , Ambrósio Sérgio R. , Arantes Andrea T. , da Silva Filho Ademar A. , Nascimento Aline N. , Costa Monique R. , Sairre Mirela I. , Veneziani Rodrigo C. S. , Magalhães Lizandra G. 

TITLE=Licochalcone a Exhibits Leishmanicidal Activity in vitro and in Experimental Model of Leishmania (Leishmania) Infantum

JOURNAL=Frontiers in Veterinary Science

VOLUME=7

YEAR=2020

URL=https://www.frontiersin.org/journals/veterinary-science/articles/10.3389/fvets.2020.00527

DOI=10.3389/fvets.2020.00527

ISSN=2297-1769

ABSTRACT=<p>The efficacy of Licochalcone A (LicoA) and its two analogs were reported against <italic>Leishmania (Leishmania) amazonensis</italic> and <italic>Leishmania (Leishmania) infantum in vitro</italic>, and in experimental model of <italic>L. (L.) infantum in vitro</italic>. Initially, LicoA and its analogs were screened against promastigote forms of <italic>L. (L.) amazonensis</italic>. LicoA was the most active compound, with IC<sub>50</sub> values of 20.26 and 3.88 μM at 24 and 48 h, respectively. Against amastigote forms, the IC<sub>50</sub> value of LicoA was 36.84 μM at 48 h. In the next step, the effectivity of LicoA was evaluated <italic>in vitro</italic> against promastigote and amastigote forms of <italic>L. (L.) infantum</italic>. Results demonstrated that LicoA exhibited leishmanicidal activity <italic>in vitro</italic> against promastigote forms with IC<sub>50</sub> values of 41.10 and 12.47 μM at 24 and 48 h, respectively; against amastigote forms the IC<sub>50</sub> value was 29.58 μM at 48 h. Assessment of cytotoxicity demonstrated that LicoA exhibited moderate mammalian cytotoxicity against peritoneal murine macrophages; the CC<sub>50</sub> value was 123.21 μM at 48 h and showed about 30% of hemolytic activity at concentration of 400 μM. <italic>L. (L.) infantum-</italic>infected hamsters and treated with LicoA at 50 mg/kg for eight consecutive days was able to significantly reduce the parasite burden in both liver and spleen in 43.67 and 39.81%, respectively, when compared with negative control group. These findings suggest that chalcone-type flavonoids can be a promising class of natural products to be considered in the search of new, safe, and effective compounds capable to treat canine visceral leishmaniosis (CVL).</p>